Synthesis and SAR of 2,4-diaminopyrimidines as potent c-jun N-terminal kinase inhibitors

被引：7

作者：

Song, Xinyi ^{[1
]}

He, Yuanjun ^{[1
]}

Koenig, Marcel ^{[1
]}

Shin, Youseung ^{[1
]}

Noel, Romain ^{[1
]}

Chen, Weimin ^{[1
]}

Ling, Yuan Yuan ^{[1
]}

Feurstein, Daniel ^{[1
]}

Lin, Li ^{[1
]}

Ruiz, Claudia H. ^{[1
]}

Cameron, Michael D. ^{[1
]}

Duckett, Derek R. ^{[1
]}

Kamenecka, Theodore M. ^{[1
]}

机构：

[1] Scripps Res Inst, Dept Mol Therapeut & Translat Res Inst, Jupiter, FL 33458 USA

来源：

MEDCHEMCOMM | 2012年 / 3卷 / 02期

关键词：

PROTEIN-KINASE; SIGNAL-TRANSDUCTION; ACTIVATION DOMAIN; PHOSPHORYLATION; STRESS; CARCINOMA; ATF-2; BINDS; JNK1;

D O I：

10.1039/c1md00219h

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The design and synthesis of a potent series of c-jun N-terminal kinase (JNK2) inhibitors is described. The development and optimization of the 2,4-diaminopyrimidines series was carried out from an earlier in-house kinase inhibitor program. Through the optimization of the scaffold 2, several cell potent compounds with good in vivo profiles were discovered.

引用

页码：238 / 243

页数：6

共 50 条

[31] Therapeutic effect of c-Jun N-terminal kinase inhibition on pancreatic cancer
Takahashi, Ryota
Hirata, Yoshihiro
Sakitani, Kosuke
Nakata, Wachiko
Kinoshita, Hiroto
Hayakawa, Yoku
Nakagawa, Hayato
Sakamoto, Kei
Hikiba, Yohko
Ijichi, Hideaki
Moses, Harold L.
Maeda, Shin
Koike, Kazuhiko
CANCER SCIENCE, 2013, 104 (03) : 337 - 344
[32] C-Jun N-terminal kinase-dependent mechanisms in respiratory disease
Bennett, B. L.
EUROPEAN RESPIRATORY JOURNAL, 2006, 28 (03) : 651 - 661
[33] c-Jun N-terminal kinases in memory and synaptic plasticity
Sherrin, Tessi
Blank, Thomas
Todorovic, Cedomir
REVIEWS IN THE NEUROSCIENCES, 2011, 22 (04) : 403 - 410
[34] c-Jun N-Terminal Kinase as a Therapeutic Target in Experimental Autoimmune Encephalomyelitis
Bagnoud, Maud
Briner, Myriam
Remlinger, Jana
Meli, Ivo
Schuetz, Sara
Pistor, Maximilian
Salmen, Anke
Chan, Andrew
Hoepner, Robert
CELLS, 2020, 9 (10)
[35] Characterization of the c-Jun N-terminal kinase-BimEL signaling pathway in neuronal apoptosis
Becker, EBE
Howell, J
Kodama, Y
Barker, PA
Bonni, A
JOURNAL OF NEUROSCIENCE, 2004, 24 (40) : 8762 - 8770
[36] Activation of c-Jun N-Terminal Kinase (JNK) during Mitosis in Retinal Progenitor Cells
Ribas, Vinicius Toledo
Goncalves, Bruno Souza
Linden, Rafael
Chiarini, Luciana Barreto
PLOS ONE, 2012, 7 (04):
[37] c-Jun N-terminal kinase/c-Jun inhibits fibroblast proliferation by negatively regulating the levels of stathmin/oncoprotein 18
Yeap, Yvonne Y. C.
Ng, Ivan H. W.
Badrian, Bahareh
Nguyen, Tuong-Vi
Yip, Yan Y.
Dhillon, Amardeep S.
Mutsaers, Steven E.
Silke, John
Bogoyevitch, Marie A.
Ng, Dominic C. H.
BIOCHEMICAL JOURNAL, 2010, 430 : 345 - 354
[38] Fish c-Jun N-Terminal Kinase (JNK) Pathway Is Involved in Bacterial MDP-Induced Intestinal Inflammation
Qu, Fufa
Xu, Wenqian
Deng, Zhangren
Xie, Yifang
Tang, Jianzhou
Chen, Zhiguo
Luo, Wenjie
Xiong, Ding
Zhao, Dafang
Fang, Jiamei
Zhou, Zhigang
Liu, Zhen
FRONTIERS IN IMMUNOLOGY, 2020, 11
[39] Inhibition of c-Jun N-terminal kinase increases apoE expression in vitro and in vivo
Pocivavsek, Ana
Rebeck, G. William
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2009, 387 (03) : 516 - 520
[40] c-Jun N-terminal phosphorylation is essential for hippocampal synaptic plasticity
Seo, Jinsoo
Hong, Jinpyo
Lee, Sung Joong
Choi, Se-Young
NEUROSCIENCE LETTERS, 2012, 531 (01) : 14 - 19

← 1 2 3 4 5 →